An investigation into the utility of a multi-compartmental, dynamic, system of the upper gastrointestinal tract to support formulation development and establish bioequivalence of poorly soluble drugs

AAPS Journal

Volumn 14, Issue 2, 2012, Pages 196-205

  Dickinson, Paul A ^a   Rmaileh, Ragheb Abu ^a   Ashworth, Lee ^a   Barker, Richard A ^a   Burke, Wendy M ^a   Patterson, Claire M ^a   Stainforth, Nick ^a   Yasin, Mohammed ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

BCS; Biopharmaceutics; Biorelevant dissolution; Bridging; Replacement

Indexed keywords

AZD 8055;

ARTICLE; BIOEQUIVALENCE; CLINICAL ARTICLE; COHORT ANALYSIS; COMPARTMENT MODEL; COMPUTER SIMULATION; COMPUTER SYSTEM; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLASSIFICATION; DRUG DOSAGE FORM COMPARISON; DRUG DOSE INCREASE; DRUG EXPOSURE; DRUG FORMULATION; DRUG RESEARCH; DRUG SOLUBILITY; DYNAMICS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; LIPID MEMBRANE; MULTIPLE DRUG DOSE; NONBIOLOGICAL MODEL; OPEN STUDY; PHASE 1 CLINICAL TRIAL; PLASMA CONCENTRATION-TIME CURVE; SINGLE DRUG DOSE; STOMACH PH; SUSPENSION; TABLET; TNO SIMULATED GASTROINTESTINAL TRACT MODEL 1; UPPER GASTROINTESTINAL TRACT;

ANIMALS; CACO-2 CELLS; CATS; CHEMISTRY, PHARMACEUTICAL; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MODELS, BIOLOGICAL; MORPHOLINES; SOLUBILITY; SWINE; THERAPEUTIC EQUIVALENCY; UPPER GASTROINTESTINAL TRACT;

EID: 84860738206     PISSN: 15507416     EISSN: None     Source Type: Journal    
DOI: 10.1208/s12248-012-9333-x     Document Type: Article

References (21)

1. Minekus M, Marteau P, Havenaar R, Huis in't Veld HJ. A multicompartmental dynamic computer-controlled model simulating the stomach and small intestine. Atla. 1995;23:197-209.
2. Havenaar R, Minekus M. In vitro model of an in vivo digestive tract. JP, US, European Patent 1994: PCT/NL93/00225
3. Blanquet S, Zeijdner E, Beyssac E, Meunier JP, Denis S, Havenaar R, Alric M. A dynamic artificial gastrointestinal system for studying the behavior of orally administered drug dosage forms under various physiological conditions. Pharm Res. 2004;21:585-91. (Pubitemid 38457280)
4. Larsson M, Minekus M, Havenaar R. Estimation of the bioavailability of iron and phosphorus in cereals using a dynamic gastrointestinal model. J Sci Food Agric. 1997;74:99-106. (Pubitemid 27236211)
5. Verwei M, Arkbage K, Havenaar R, Van den Berg H, Witthöft C, Schaafsma G. Folic acid and 5-methyl-tetrahydrofolate in fortified milk are bioaccessible as determined in a dynamic in vitro gastrointestinal model. J Nutr. 2003;133:2377-83. (Pubitemid 36841568)
6. Krul CAM, Luiten-Schuite Baan AR, Verhagen H, Mohn G, Feron V, Havenaar R. Application of a dynamic in vitro gastrointestinal tract model to study the availability of food mutagens, using heterocyclic aromatic amines as model compounds. Food Chem Toxicol. 2000;38:783-92. (Pubitemid 30628873)
7. Marteau P, Minekus M, Havenaar R, Huis in't Veld JHJ. Survival of lactic acid bacteria in a dynamic model of the stomach and small intestine: validation and the effects of the bile. J Dairy Sci. 1997;80:1031-7. (Pubitemid 127447084)
8. Blanquet S, Meunier JP, Minekus M, Marol-Bonnin S, Alric M. Recombinant Saccharomyces cerevisiae expressing a P450 in artificial digestive systems: a model for biodetoxication in the human digestive environment. Appl Env Microbiol. 2003;69:2884-92. (Pubitemid 36560370)
9. OomenA, HackA, MinekusM, ZeijdnerE, CorneliusC, Schoeters G, Verstraete W, Van deWiele T, Wragg J, Romplelberg CJM, Sips AJAM, Van Wijnen JH. Comparison of five in vitro digestion models to study the bioaccessibility of soil contaminants. Environ Sci Tech. 2002;36:3326-34. (Pubitemid 34847602)
10. Cardot J-M, Beyssac E and Alric M. In vitro-in vivo correlation: importance of dissolution in IVIVC. Dissolution Tech. 2007; pp 15-19.
11. Polli JE. In vitro studies are sometimes better than conventional human pharmacokinetic in vivo studies in assessing bioequiva-lence of immediate-release solid oral dosage forms. AAPS J. 2008;10:289-99.
12. Naylor TA, Connolly PG, Martini LG, Elder DP, Minekus M, Havenaar R and Zeijdner E. Use of a gastro-intestinal model and Gastroplus™ for the prediction of in vivo performance. Industrial Pharm. 2006; 9-12.
13. Souliman S, Blanquet S, Beyssac E, Cardot J-M. A level A in vitro/in vivo correlation in fasted and fed states using different methods: applied to solid release oral dosage form. Eur J Pharm Sci. 2006;27:72-9. (Pubitemid 41728257)
14. Tenjatla S, Romasanat V, Zeijdner E, Villa R, Moro L. Release of 5-aminosalicylate from MMX Mesalamine tablet during transit though a simulated gastrointestinal tract system. Adv Ther. 2007;24:826-39.
15. Fadda HM, Merchant HA, Arafat BT, Basit AW. Physiological bicarbonate buffers: stabilisation and use as dissolution media for modified release systems. Int J Pharm. 2009;382:56-60.
16. Selen A, Cruañes MT, Müllertz A, Dickinson PA, Cook JA, Polli JE, Kesisoglou F, Crison J, Johnson KC, Muirhead GT, Schofield T, Tsong Y. Conference report: applied biopharmaceutics and quality by design for dissolution/release specification setting: product quality for patient benefit. AAPS J. 2010;12:465-72.
17. Reis PM, Raab TW, Chuat JY, Leser ME, Miller R, Watzke HJ, Homberg K. Influence of surfactants on lipase fat digestion in a model gastro-intestinal system. Food Biophys. 2008;3:370-81.
18. Morihara M, Aoyagi N, Kaniwa N, Kojima S, Ogata H. Assessment of gastric acidity of Japanese subjects over the last 15 years. Biol Pharm Bull. 2001;24:313-5. (Pubitemid 32237176)
19. Waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a Biophar-maceutics Classification System. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER). http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/ Guidances/ucm070246.pdf). Accessed 18 Jan, 2012.
20. Naing A, Aghajanian C, Raymond E Kurzrock R, Blanco M, Oelmann E, Grinsted L, Burke W, Kaye S, Banerji U. First results from a phase I trial of AZD8055, a dual mTORC1 and mTORC2 inhibitor. Mol Cancer Ther. 2011;10 (11 Suppl): Abstract nr A168.
21. McAllister M. Dynamic dissolution: a step closer to predictive dissolution testing? Mol Pharm. 2010;7:1374-87.